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Novel indium-111 labeled gastrin peptide analogues (MG-CL1-4): synthesis and quality control.

Abstract
Radiolabeled neuropeptides are widely investigated to diagnose and therapy of tumors. These peptides get internalization after binding with particular receptors at the surface of cells and finally move to lysosome. Internalization into tumor cells helps in mapping the infected site. Minigastrin peptide analogues (MG-CL1-4) were synthesised and labeled with 111-In radioisotope under different sets of conditions for imaging CCk-2 receptor bearing tumors. Different parameters such as temperature (80-100°C), pH (4-12), incubation time (5-30 minutes) and dilution effect were investigated to get the maximum labeling yield and stability. The results indicated that MG-CL1-4 is successfully labeled with indium-111 at pH 4.5 with heating at 98°C for 15 minute. At these conditions i.e. heating, pH and incubation minimum oxidized and maximum labeling yield, more than 94 %, was obtained. The labeling stability was studied by incubating the radiolabeled complex for predefined time points in PBSA and blood serum. Results show that more than 90% radiolabeled MG-CL1-4 remained intact.
AuthorsSyed Ali-Raza Naqvi, Zulfiqar Ali Khan, Saeed Ahmad Nagra, Muhammad Yar, Tauqir A Sherazi, Sohail Shahzad Shahzad, Syed Qaiser Shah, Nasir Mahmood, Malik Muhammad Ishfaq, Stephen John Mather
JournalPakistan journal of pharmaceutical sciences (Pak J Pharm Sci) Vol. 26 Issue 2 Pg. 299-305 (Mar 2013) ISSN: 1011-601X [Print] Pakistan
PMID23455200 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Gastrins
  • Indium Radioisotopes
  • minigastrin
Topics
  • Gastrins (blood, chemical synthesis, standards)
  • Humans
  • Hydrogen-Ion Concentration
  • Indium Radioisotopes
  • Isotope Labeling (standards)
  • Oxidation-Reduction
  • Protein Stability
  • Quality Control
  • Temperature
  • Time Factors

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